DDR-TRK-1 (DDR1 inhibitor 6j)
- Product Name
- DDR-TRK-1 (DDR1 inhibitor 6j)
- CAS No.
- 1934246-19-1
- Chemical Name
- DDR-TRK-1 (DDR1 inhibitor 6j)
- Synonyms
- DDR-TRK-1;DDRTRK1,DDR TRK 1;DDR-TRK-1, 10 mM in DMSO;DDR-TRK-1 (DDR1 inhibitor 6j);7-Isoquinolinecarboxamide, 1,2,3,4-tetrahydro-4-methyl-N-[3-(4-methyl-1H-imidazol-1-yl)-5-(trifluoromethyl)phenyl]-2-(5-pyrimidinyl)-, (4R)-
- CBNumber
- CB24844697
- Molecular Formula
- C26H23F3N6O
- Formula Weight
- 492.5
- MOL File
- 1934246-19-1.mol
DDR-TRK-1 (DDR1 inhibitor 6j) Property
- Boiling point:
- 609.3±55.0 °C(Predicted)
- Density
- 1.37±0.1 g/cm3(Predicted)
- storage temp.
- Store at -20°C
- solubility
- Soluble in DMSO
- pka
- 12.84±0.70(Predicted)
- form
- powder
- color
- white to beige
- optical activity
- [α]/D -25 to -20°, c =0.5 in methanol
DDR-TRK-1 (DDR1 inhibitor 6j) Chemical Properties,Usage,Production
Uses
DDR-TRK-1 is a selective Discoidin Domain Receptor 1 (DDR1) inhibitor, with an IC50 value of 9.4 nM. DDR-TRK-1 also inhibits TRK family.
Biological Activity
DDR-TRK-1 was shown to inhibit the kinase activity of Discoidin Domain Receptor 1 (DDR1) with an IC50 value of 9.4 nM. DDR receptors are linked to the progression of various human diseases, including fibrotic disorders such as pulmonary fibrosis, as well as atherosclerosis and cancer. DDR-TRK-1 showed a therapeutic effect in a mouse model of pulmonary fibrosis and inhibited Panc-1 pancreatic cancer cell colony formation and migration. DDR-TRK-1 also inhibits the TRK family kinases TRKA, TRKB, and TRKC, which are selectively expressed in neuronal tissue. DDR-TRK-1N is the negative control compound.
in vivo
DDR-TRK-1 prevents these BLM-induced pathological changes in a dose-dependent manner. These results agree with the expression levels of fibrotic markers in lung tissue lysates, including fibronectin and α-smooth muscle actin (SMA). Further analyses also reveal that the administration of DDR-TRK-1 cause a dose-dependent suppression in the content of hydroxyproline, a unique amino acid found in collagen. The above data collectively indicate the promising therapeutic potential of DDR-TRK-1 against the BLM-induced pulmonary fibrosis[1].
References
[1] Zhen Wang, et al. Structure-Based Design of Tetrahydroisoquinoline-7-carboxamides as Selective Discoidin Domain Receptor 1 (DDR1) Inhibitors. J Med Chem. 2016 Jun 23; 59(12): 5911–5916. DOI:10.1021/acs.jmedchem.6b00140
DDR-TRK-1 (DDR1 inhibitor 6j) Preparation Products And Raw materials
Raw materials
Preparation Products
DDR-TRK-1 (DDR1 inhibitor 6j) Suppliers
- Tel
- +1-781-999-5354; +17819995354
- marketing@targetmol.com
- Country
- United States
- ProdList
- 32435
- Advantage
- 58
- Tel
- +1-781-999-5354;
- support@targetmol.com
- Country
- United States
- ProdList
- 39035
- Advantage
- 58
- Tel
- --
- Fax
- --
- sales@medchemexpress.com
- Country
- United States
- ProdList
- 6398
- Advantage
- 58